Overview
- Gronlien, J.H. et al. (2007) Mol. Pharmacol. 72, 715.
- Hurst, R.S. et al. (2005) J. Neurosci. 25, 4396.
- Kalappa, B.I. et al. (2013) Br. J. Pharmacol. 169, 1862.
Alomone Labs PNU-120596 positively modulates α7 nAChR expressed in Xenopus oocytes.A. Representative time course of PNU-120596 (#P-350) effect on α7 current, elicited every 100 sec by transient applications of 50 µM acetylcholine, while membrane potential was held at -80 mV. Current significantly enhanced after a 60 sec pre-application of 3 µM PNU-120596 (green bar). B. Superimposed traces of α7 currents before (black) and after (green) application of 3 µM PNU-120596, which enhanced the current evoked by acetylcholine stimulation (arrow). Taken from the experiment in A.
PNU-120596 is as a potent and selective positive allosteric modulator of α7 nicotinic acetylcholine receptors (nAChRs). It potentiates nAChR α7 currents in Xenopus oocytes and in SH-EP1 cells with EC50 values of 1.6 µM and 216 nM, respectively1-2. The compound displays neuroprotective characteristics in vivo and has the ability to increase the potency and maximal efficacy of agonists and to prolong the duration of the agonist-evoked macroscopic currents1,2.
nAChRs receptors are responsible for mediating the effects of the neurotransmitter acetylcholine (ACh). They play critical roles in the central and peripheral nervous system where they regulate neurotransmitter release, cell excitability, neuronal integration. They are involved in functions such as sleep and arousal patterns, fatigue, hunger, anxiety, and pain processing2,3,4.
